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Tazemetostat + abiraterone + prednisone is an investigational combination regimen under clinical evaluation for the treatment of metastatic castration-resistant prostate cancer (mCRPC). **Tazemetostat** is an oral, small molecule inhibitor of the histone methyltransferase **EZH2** (Enhancer of Zeste Homolog 2), developed to target epigenetic modulation in cancer cells. **Abiraterone** is an androgen biosynthesis inhibitor that selectively inhibits **CYP17A1**, reducing androgen and cortisol production, and is used in combination with **prednisone**, a synthetic glucocorticoid, to prevent mineralocorticoid excess and associated adverse events. This combination is being evaluated to determine if EZH2 inhibition can overcome resistance to androgen-signaling inhibitors, potentially improving efficacy in patients with mCRPC who have progressed on prior anti-androgen therapies[1][2][4].
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